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Items: 1 to 20 of 99

1.

Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis.

Weinstabl H, Treu M, Rinnenthal J, Zahn SK, Ettmayer P, Bader G, Dahmann G, Kessler D, Rumpel K, Mischerikow N, Savarese F, Gerstberger T, Mayer M, Zoephel A, Schnitzer R, Sommergruber W, Martinelli P, Arnhof H, Peric-Simov B, Hofbauer KS, Garavel G, Scherbantin Y, Mitzner S, Fett TN, Scholz G, Bruchhaus J, Burkard M, Kousek R, Ciftci T, Sharps B, Schrenk A, Harrer C, Haering D, Wolkerstorfer B, Zhang X, Lv X, Du A, Li D, Li Y, Quant J, Pearson M, McConnell DB.

J Med Chem. 2019 Sep 12;62(17):7976-7997. doi: 10.1021/acs.jmedchem.9b00718. Epub 2019 Aug 14.

PMID:
31365252
2.

Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells.

Mullarky E, Xu J, Robin AD, Huggins DJ, Jennings A, Noguchi N, Olland A, Lakshminarasimhan D, Miller M, Tomita D, Michino M, Su T, Zhang G, Stamford AW, Meinke PT, Kargman S, Cantley LC.

Bioorg Med Chem Lett. 2019 Sep 1;29(17):2503-2510. doi: 10.1016/j.bmcl.2019.07.011. Epub 2019 Jul 6.

PMID:
31327531
3.

Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers.

Mullarky E, Lucki NC, Beheshti Zavareh R, Anglin JL, Gomes AP, Nicolay BN, Wong JC, Christen S, Takahashi H, Singh PK, Blenis J, Warren JD, Fendt SM, Asara JM, DeNicola GM, Lyssiotis CA, Lairson LL, Cantley LC.

Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):1778-83. doi: 10.1073/pnas.1521548113. Epub 2016 Feb 1. Erratum in: Proc Natl Acad Sci U S A. 2016 Mar 15;113(11):E1585.

4.

Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors.

Rohde JM, Brimacombe KR, Liu L, Pacold ME, Yasgar A, Cheff DM, Lee TD, Rai G, Baljinnyam B, Li Z, Simeonov A, Hall MD, Shen M, Sabatini DM, Boxer MB.

Bioorg Med Chem. 2018 May 1;26(8):1727-1739. doi: 10.1016/j.bmc.2018.02.016. Epub 2018 Feb 27.

5.

The NAD+ Salvage Pathway Supports PHGDH-Driven Serine Biosynthesis.

Murphy JP, Giacomantonio MA, Paulo JA, Everley RA, Kennedy BE, Pathak GP, Clements DR, Kim Y, Dai C, Sharif T, Gygi SP, Gujar S.

Cell Rep. 2018 Aug 28;24(9):2381-2391.e5. doi: 10.1016/j.celrep.2018.07.086.

6.

Validating and enabling phosphoglycerate dehydrogenase (PHGDH) as a target for fragment-based drug discovery in PHGDH-amplified breast cancer.

Unterlass JE, Baslé A, Blackburn TJ, Tucker J, Cano C, Noble MEM, Curtin NJ.

Oncotarget. 2016 Aug 22;9(17):13139-13153. doi: 10.18632/oncotarget.11487. eCollection 2018 Mar 2.

7.

Structural insights into the enzymatic activity and potential substrate promiscuity of human 3-phosphoglycerate dehydrogenase (PHGDH).

Unterlass JE, Wood RJ, Baslé A, Tucker J, Cano C, Noble MME, Curtin NJ.

Oncotarget. 2017 Nov 6;8(61):104478-104491. doi: 10.18632/oncotarget.22327. eCollection 2017 Nov 28.

8.

3-Phosphoglycerate Transhydrogenation Instead of Dehydrogenation Alleviates the Redox State Dependency of Yeast de Novo l-Serine Synthesis.

Paczia N, Becker-Kettern J, Conrotte JF, Cifuente JO, Guerin ME, Linster CL.

Biochemistry. 2019 Jan 29;58(4):259-275. doi: 10.1021/acs.biochem.8b00990. Epub 2019 Jan 22.

PMID:
30668112
9.

Rational Design of Selective Allosteric Inhibitors of PHGDH and Serine Synthesis with Anti-tumor Activity.

Wang Q, Liberti MV, Liu P, Deng X, Liu Y, Locasale JW, Lai L.

Cell Chem Biol. 2017 Jan 19;24(1):55-65. doi: 10.1016/j.chembiol.2016.11.013. Epub 2016 Dec 29.

10.

A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate.

Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu-Remaileh M, Shaul YD, Liu CM, Zhou M, Koh MJ, Chung H, Davidson SM, Luengo A, Wang AQ, Xu X, Yasgar A, Liu L, Rai G, Westover KD, Vander Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM.

Nat Chem Biol. 2016 Jun;12(6):452-8. doi: 10.1038/nchembio.2070. Epub 2016 Apr 25. Erratum in: Nat Chem Biol. 2016 Jul 19;12 (8):656.

11.

Functional genomics reveal that the serine synthesis pathway is essential in breast cancer.

Possemato R, Marks KM, Shaul YD, Pacold ME, Kim D, Birsoy K, Sethumadhavan S, Woo HK, Jang HG, Jha AK, Chen WW, Barrett FG, Stransky N, Tsun ZY, Cowley GS, Barretina J, Kalaany NY, Hsu PP, Ottina K, Chan AM, Yuan B, Garraway LA, Root DE, Mino-Kenudson M, Brachtel EF, Driggers EM, Sabatini DM.

Nature. 2011 Aug 18;476(7360):346-50. doi: 10.1038/nature10350.

12.

Inhibition of Phosphoglycerate Dehydrogenase Attenuates Bleomycin-induced Pulmonary Fibrosis.

Hamanaka RB, Nigdelioglu R, Meliton AY, Tian Y, Witt LJ, O'Leary E, Sun KA, Woods PS, Wu D, Ansbro B, Ard S, Rohde JM, Dulin NO, Guzy RD, Mutlu GM.

Am J Respir Cell Mol Biol. 2018 May;58(5):585-593. doi: 10.1165/rcmb.2017-0186OC.

13.

Phosphoglycerate dehydrogenase promotes pancreatic cancer development by interacting with eIF4A1 and eIF4E.

Ma X, Li B, Liu J, Fu Y, Luo Y.

J Exp Clin Cancer Res. 2019 Feb 11;38(1):66. doi: 10.1186/s13046-019-1053-y.

14.

An epitope tag alters phosphoglycerate dehydrogenase structure and impairs ability to support cell proliferation.

Mattaini KR, Brignole EJ, Kini M, Davidson SM, Fiske BP, Drennan CL, Vander Heiden MG.

Cancer Metab. 2015 Apr 29;3:5. doi: 10.1186/s40170-015-0131-7. eCollection 2015.

15.

Human phosphoglycerate dehydrogenase produces the oncometabolite D-2-hydroxyglutarate.

Fan J, Teng X, Liu L, Mattaini KR, Looper RE, Vander Heiden MG, Rabinowitz JD.

ACS Chem Biol. 2015 Feb 20;10(2):510-6. doi: 10.1021/cb500683c. Epub 2014 Nov 18.

16.

Kinetic mechanism of the endogenous lactate dehydrogenase activity of duck epsilon-crystallin.

Chang GG, Huang SM, Chiou SH.

Arch Biochem Biophys. 1991 Feb 1;284(2):285-91.

PMID:
1989512
17.

Overcoming erlotinib resistance in EGFR mutation-positive lung adenocarcinomas through repression of phosphoglycerate dehydrogenase.

Dong JK, Lei HM, Liang Q, Tang YB, Zhou Y, Wang Y, Zhang S, Li WB, Tong Y, Zhuang G, Zhang L, Chen HZ, Zhu L, Shen Y.

Theranostics. 2018 Feb 12;8(7):1808-1823. doi: 10.7150/thno.23177. eCollection 2018.

18.

Serine synthesis through PHGDH coordinates nucleotide levels by maintaining central carbon metabolism.

Reid MA, Allen AE, Liu S, Liberti MV, Liu P, Liu X, Dai Z, Gao X, Wang Q, Liu Y, Lai L, Locasale JW.

Nat Commun. 2018 Dec 21;9(1):5442. doi: 10.1038/s41467-018-07868-6.

19.

p53 Protein-mediated regulation of phosphoglycerate dehydrogenase (PHGDH) is crucial for the apoptotic response upon serine starvation.

Ou Y, Wang SJ, Jiang L, Zheng B, Gu W.

J Biol Chem. 2015 Jan 2;290(1):457-66. doi: 10.1074/jbc.M114.616359. Epub 2014 Nov 17.

20.

A novel small-molecule inhibitor of 3-phosphoglycerate dehydrogenase.

Mullarky E, Lairson LL, Cantley LC, Lyssiotis CA.

Mol Cell Oncol. 2016 Mar 30;3(4):e1164280. doi: 10.1080/23723556.2016.1164280. eCollection 2016 Jul.

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